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Mass spectrometry enables the discovery of inhibitors of an LPS transport assembly via disruption of protein-protein interactions.
Fiorentino, Francesco; Rotili, Dante; Mai, Antonello; Bolla, Jani R; Robinson, Carol V.
Afiliación
  • Fiorentino F; Physical and Theoretical Chemistry Laboratory, Department of Chemistry, University of Oxford, Oxford, OX1 3QZ, UK. jani.bolla@chem.ox.ac.uk.
  • Rotili D; The Kavli Institute for Nanoscience Discovery, 3 South Parks Road, Oxford, OX1 3QU, UK.
  • Mai A; Department of Drug Chemistry & Technologies, Sapienza University of Rome, P. le A Moro 5, Rome 00185, Italy. antonello.mai@uniroma1.it.
  • Bolla JR; Department of Drug Chemistry & Technologies, Sapienza University of Rome, P. le A Moro 5, Rome 00185, Italy. antonello.mai@uniroma1.it.
  • Robinson CV; Physical and Theoretical Chemistry Laboratory, Department of Chemistry, University of Oxford, Oxford, OX1 3QZ, UK. jani.bolla@chem.ox.ac.uk.
Chem Commun (Camb) ; 57(82): 10747-10750, 2021 Oct 14.
Article en En | MEDLINE | ID: mdl-34585198
ABSTRACT
We developed a native mass spectrometry-based approach to quantify the monomer-dimer equilibrium of the LPS transport protein LptH. We use this method to assess the potency and efficacy of an antimicrobial peptide and small molecule disruptors, obtaining new information on their structure-activity relationships. This approach led to the identification of quinoline-based hit compounds representing the basis for the development of novel LPS transport inhibitors.
Asunto(s)

Texto completo: 1 Colección: 01-internacional Asunto principal: Péptidos / Quinolinas / Receptores de Lipopolisacáridos / Bibliotecas de Moléculas Pequeñas / Antiinfecciosos Límite: Humans Idioma: En Revista: Chem Commun (Camb) Asunto de la revista: QUIMICA Año: 2021 Tipo del documento: Article País de afiliación: Reino Unido

Texto completo: 1 Colección: 01-internacional Asunto principal: Péptidos / Quinolinas / Receptores de Lipopolisacáridos / Bibliotecas de Moléculas Pequeñas / Antiinfecciosos Límite: Humans Idioma: En Revista: Chem Commun (Camb) Asunto de la revista: QUIMICA Año: 2021 Tipo del documento: Article País de afiliación: Reino Unido